Polymorphism and crystallization of active pharmaceutical ingredients (APIs).

Abstract:

:Active pharmaceutical ingredients (APIs), frequently delivered to the patient in the solid-state as part of an approved dosage form, can exist in such diverse solid forms as polymorphs, pseudopolymorphs, salts, co-crystals and amorphous solids. Various solid forms often display different mechanical, thermal, physical and chemical properties that can remarkably influence the bioavailability, hygroscopicity, stability and other performance characteristics of the drug. Hence, a thorough understanding of the relationship between the particular solid form of an active pharmaceutical ingredient (API) and its functional properties is important in selecting the most suitable form of the API for development into a drug product. In past decades, there have been significant efforts on the discovery, selection and control of the solid forms of APIs and bulk drugs. This contribution discusses the thermodynamics and kinetics of polymorphic systems, the characterization of polymorphs, and the transformation between polymorphs. The major techniques for polymorph discovery and control developed in the past years are discussed as well.

journal_name

Curr Med Chem

authors

Lu J,Rohani S

doi

10.2174/092986709787549299

subject

Has Abstract

pub_date

2009-01-01 00:00:00

pages

884-905

issue

7

eissn

0929-8673

issn

1875-533X

journal_volume

16

pub_type

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